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Varlitinib (ARRY-543; ASLAN-001) is a novel, potent, orally bioavailable, selective and reversible ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Varlitinib reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types.
| ln Vitro |
In cellular experiments employing tumor cells overexpressing EGFR (A431) or ErbB-2 (BT474), varlitinib tosylate (ARRY-334543) potently suppresses substrate phosphorylation. When evaluated against a panel of 104 disruptions, varlitinib tosylate was shown to be highly potent against EGFR/ErbB-2 and did not exhibit any substantial action [2].
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| ln Vivo |
At a dose of 100 mg/kg twice day, varlitinib tosylate completely suppressed the growth of the tumor. The phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomes, 4EBP1, Cdk-2, Cdc-2, and apoptotic blastoma was significantly suppressed five days following therapy with varlitinib tosylate. Treatment with varlitinib tosylate caused the caspase 3 transporter to rise and survivin to significantly decline [1]. In a mouse xenograft model, varlitinib tosylate (25, 50, and 100 mg/kg) showed a noteworthy dose-related reduction of tumor growth in A431-derived tumors when given twice a day for 21 days [2].
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| References |
[1]. Hsieh C, et al. Varlitinib to demonstrate anti-tumour efficacy in patient-derived hepatocellular carcinoma xenograft models. Journal of Clinical Oncology 34, no. 15_suppl
[2]. Miknis G, et al. ARRY-334543, A potent, orally active small molecule inhibitor of EGFR and ErbB-2.Proc Amer Assoc Cancer Res, Volume 46, 2005 |
| Molecular Formula |
C36H35CLN6O8S3
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|---|---|
| Molecular Weight |
88.9059
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| CAS # |
1146629-86-8
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| Related CAS # |
Varlitinib;845272-21-1
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| SMILES |
C[C@H]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O
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| InChi Key |
QSUPQMGDXOHVLK-FFXKMJQXSA-N
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| InChi Code |
InChI=1S/C22H19ClN6O2S.2C7H8O3S/c1-13-10-31-22(27-13)29-14-2-4-18-16(8-14)21(26-12-25-18)28-15-3-5-19(17(23)9-15)30-11-20-24-6-7-32-202*1-6-2-4-7(5-3-6)11(8,9)10/h2-9,12-13H,10-11H2,1H3,(H,27,29)(H,25,26,28)2*2-5H,1H3,(H,8,9,10)/t13-/m1../s1
|
| Chemical Name |
4-N-[3-Chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine4-methylbenzenesulfonic
acid
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| Synonyms |
ARRY-543 ASLAN-001ARRY543 ASLAN001ARRY 543 ASLAN 001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 11.2473 mL | 56.2366 mL | 112.4733 mL | |
| 5 mM | 2.2495 mL | 11.2473 mL | 22.4947 mL | |
| 10 mM | 1.1247 mL | 5.6237 mL | 11.2473 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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